产品
编 号：F297736
分子式：C26H25F9N2O4
分子量：600.47
分子式：C26H25F9N2O4
分子量：600.47
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是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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CAS No: 262352-17-0
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生物活性：
Torcetrapib (CP-529414) is a selective, potent cholesteryl ester transfer protein (CETP) inhibitor. A typical inhibition curve for whole human plasma, having a CETP concentration of 37 nM.
体内研究：
Torcetrapib (3, 10, or 30 mg/kg every day [qd]; oral gavage for 14 days) significantly increases high-density lipoprotein (HDL) cholesterol and reduceslow-density lipoprotein (LDL) cholesterol, and there is a tendency for Torcetrapib to reduce very-low-density lipoprotein (VLDL) cholesterol and triglycerides. Maximal increase in HDL cholesterol is 53% with Torcetrapib.Animal Model:Male Tg (B6; SJL-TgN (CETP)-TgN (ApoB100)) mice at 6 to 7 weeks of age
Dosage:3, 10, and 30 mg/kg
Administration:Orally every day for 14 days
Result:Significantly Increased HDL cholesterol by 27%, 24%, and 53% in the 3, 10, and 30 mg/kg groups compared to baseline, respectively, after 14 days of treatment. Significantly decreased LDL cholesterol by 44% and 35% at 10 and 30 mg/kg compared to baseline, respectively, after 14 days of treatment.
体外研究：
The IC50 for Torcetrapib determined from the linear portion of the curves (25 to 80 nM) is 52 and 65 nM for the 3H-HDL and 14C-LDL cholesteryl ester transfer assays, respectively, using the specific activity-adjusted calculation, and 47 and 61 nM using a single exponential decay function.Torcetrapib (0, 0.5, 1, 5, and 10 μM) significantly reduced MCF-7 cells growth.Torcetrapib (0, 1, 5, 10, and 20 μM) does not inducing MCF-7 cells apoptosis.Torcetrapib (10 μM) binds to CETP with high affinity and down-regulates CETP expression.
Torcetrapib (CP-529414) is a selective, potent cholesteryl ester transfer protein (CETP) inhibitor. A typical inhibition curve for whole human plasma, having a CETP concentration of 37 nM.
体内研究：
Torcetrapib (3, 10, or 30 mg/kg every day [qd]; oral gavage for 14 days) significantly increases high-density lipoprotein (HDL) cholesterol and reduceslow-density lipoprotein (LDL) cholesterol, and there is a tendency for Torcetrapib to reduce very-low-density lipoprotein (VLDL) cholesterol and triglycerides. Maximal increase in HDL cholesterol is 53% with Torcetrapib.Animal Model:Male Tg (B6; SJL-TgN (CETP)-TgN (ApoB100)) mice at 6 to 7 weeks of age
Dosage:3, 10, and 30 mg/kg
Administration:Orally every day for 14 days
Result:Significantly Increased HDL cholesterol by 27%, 24%, and 53% in the 3, 10, and 30 mg/kg groups compared to baseline, respectively, after 14 days of treatment. Significantly decreased LDL cholesterol by 44% and 35% at 10 and 30 mg/kg compared to baseline, respectively, after 14 days of treatment.
体外研究：
The IC50 for Torcetrapib determined from the linear portion of the curves (25 to 80 nM) is 52 and 65 nM for the 3H-HDL and 14C-LDL cholesteryl ester transfer assays, respectively, using the specific activity-adjusted calculation, and 47 and 61 nM using a single exponential decay function.Torcetrapib (0, 0.5, 1, 5, and 10 μM) significantly reduced MCF-7 cells growth.Torcetrapib (0, 1, 5, 10, and 20 μM) does not inducing MCF-7 cells apoptosis.Torcetrapib (10 μM) binds to CETP with high affinity and down-regulates CETP expression.
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